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Cat. No. Product Name CAS No. Information
PC-35732

PLB-1001

1440964-89-5

PLB-1001 (Bozitinib, PLB1001, CBI-3103, CBT-101) is a potent, highly selective, ATP-competitive, BBB-permeable MET kinase inhibitor, potently inhibits MET activity by 95.1% at 2 uM; Similar with crizotinib, PLB-1001 inhibited the phosphorylation of MET and STAT3, indicating a robust inhibitory effect of PLB-1001 on MET and its downstream signaling pathways; demonstrates remarkable potency in selectively inhibiting MET-altered tumor cells (METex14) in preclinical models; also exhibits clinical potential for precisely treating gliomas.

Liver Cancer

Phase 2 Clinical

PC-43511

Capmatinib

1029712-80-8

Capmatinib (INCB-28060, INC-280) is a highly potent, selective, ATP competitive inhibitor of c-MET kinase with IC50 of 0.13 nM, displays no activity against RONβ, EGFR and HER-3; inhibits c-MET phosphorylation (IC50=1 nM) in SNU-5 human gastric cancer cell line, is slightly more potent in H596 and H1437 lung cancer cell lines that express mutant c-MET due to an exon 14 deletion and a R988C mutation; inhibits c-MET phosphorylation and tumor growth in c-MET-driven mouse tumor models.

Lung Cancer

Phase 3 Clinical

PC-43478

MK-8033 hydrochloride

1283000-43-0

MK-8033 is a potent, specific, dual c-Met/Ron kinases inhibitor with IC50 of 1/7 nM, also potently inhibits oncogenic c-Met activation loop mutants Y1230C, Y1230H and Y1235D with IC50 of 0.6-1.2 nM; MK-8033 is >100-fold selective relative to Ron and c-Met inhibition against a panel of 221 kinases; potently and selectively inhibits growth in c-Met amplified cell lines (GTL-16 proliferation IC50 =582 nM), causes full inhibition of tumor growth in c-Met amplified (GTL-16) subcutaneous tumor xenograft model; synergizes with carboplatin plus paclitaxel to inhibit ovarian cancer cell growth.

Solid Tumors

Phase 1 Clinical

PC-43477

MK-8033

1001917-37-8

MK-8033 is a potent, specific, dual c-Met/Ron kinases inhibitor with IC50 of 1/7 nM, also potently inhibits oncogenic c-Met activation loop mutants Y1230C, Y1230H and Y1235D with IC50 of 0.6-1.2 nM; MK-8033 is >100-fold selective relative to Ron and c-Met inhibition against a panel of 221 kinases; potently and selectively inhibits growth in c-Met amplified cell lines (GTL-16 proliferation IC50 =582 nM), causes full inhibition of tumor growth in c-Met amplified (GTL-16) subcutaneous tumor xenograft model; synergizes with carboplatin plus paclitaxel to inhibit ovarian cancer cell growth.

Solid Tumors

Phase 1 Clinical

PC-63402

JNJ-38877618

943540-74-7

JNJ-38877618 (OMO-1) is a novel potent, highly selective, orally bioavailable c-Met tyrosine kinase inhibitor with Kd of 1.2, 2.1 and 21 nM for WT, M1250T and Y1235D mutants MET, respectively; potently inhibits MET receptor phosphorylation and downstream pathway modulation in the nanomolar range and induces anti-proliferative and anti-migratory activity in models with MET gene amplification, mutant or ligand-mediated pathway activation; completely suppresses tumour growth SNU5 MET amplified gastric, U87-MG HGF autocrine glioblastoma and Hs746T MET exon 14 skipping mutant gastric cancer models.

Solid Tumors

Phase 1 Clinical

PC-42888

BMS 777607

1025720-94-8

BMS 777607 is a potent, selective, orally efficacious inhibitor of Met kinase with IC50 of 3.9 nM, also potently inhibits Ron, Axl, Tyro-3 and Mer (IC50<15 nM), 40-fold selectivity over Lck, VEGFR-2 and TrkA/B; inhibits cell scattering activated by exogenous HGF in c-Met-expressing PC-3 and DU145 prostate cancer cells, suppresses HGF-stimulated cell migration and invasion with IC50 of <0.1 uM; potently blocks HGF-stimulated c-Met autophosphorylation and downstream activation of Akt and ERK at nanomolar level; demonstrates complete tumor stasis in Met-dependent GTL-16 human gastric carcinoma xenograft models.

Gastric Cancer

Phase 2 Clinical

PC-70080

Glesatinib

936694-12-1

Glesatinib (MGCD-265) is a tyrosine kinase inhibitor that potently and selectively inhibits Met and Axl kinase.

Lung Cancer

Phase 2 Clinical

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